SYNTHESIS AND BIOLOGICAL-ACTIVITY OF NK1 SUBSTANCE-P SELECTIVE AGONISTS BY MODIFYING THE METHIONYL RESIDUE

Authors
POULOS C ANTONIOU M PATACCHINI R MAGGI CA PEGORARO S ROVERO P
Citation
C. Poulos et al., SYNTHESIS AND BIOLOGICAL-ACTIVITY OF NK1 SUBSTANCE-P SELECTIVE AGONISTS BY MODIFYING THE METHIONYL RESIDUE, Neuropeptides, 27(1), 1994, pp. 27-29
Citations number
7
Categorie Soggetti
Neurosciences,"Endocrynology & Metabolism
Journal title
Neuropeptides → ACNP
ISSN journal
01434179
Volume
27
Issue
1
Year of publication
1994
Pages
27 - 29
Database
ISI
SICI code
0143-4179(1994)27:1<27:SABONS>2.0.ZU;2-9
Abstract
A series of analogues of substance P, where the Met(11) residue was re placed by Glu(OCH2CH3), Glu(OBzl) and Hse(CH3), were synthesized in or der to investigate the effect on agonist activity of modifications at the C-terminal residue. The biological activities in the guinea-pig il eum assay (NK1 receptor) and rat pulmonary artery (NK2 receptor) indic ate that replacement of the SCH3 group of Met(11) of substance P by th e COOBzl or OCH3 groups favour interaction with the NK1 receptor and i ncrease selectivity towards this receptor subtype.